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Nifedipine controlled-release tablet composition and preparation method thereof

A technology for nifedipine and composition, applied in the field of nifedipine controlled-release tablet composition and preparation thereof, can solve the problems of complicated preparation process, long drying time, slow water absorption speed and hydration speed of polyoxyethylene, and avoid the Pigment and toxic solvent, simple and easy preparation process, good release curve effect

Active Publication Date: 2017-01-25
浙江为康制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Nifedipine push-pull osmotic pump controlled-release tablet is composed of a double-layer tablet core composed of a drug-containing layer and a booster layer and a semi-permeable membrane controlled-release coating. Lasers are used to make small holes for drug release on the drug-containing coating film. The preparation process is complicated, the production equipment is expensive, the precision is high, the operation is inconvenient, the production cycle is long, the production cost is high, and materials that are harmful to the body and the environment such as pigments and acetone are used in the production process
[0003] Polyoxyethylene (PEO) is a hydrophilic polymer material. For the poorly soluble drug nifedipine, the matrix is ​​mainly eroded, and it has attracted more and more attention from the pharmaceutical community in oral gel matrix tablets. There are some inherent disadvantages: the water absorption rate and hydration rate of polyoxyethylene are slow, so the time lag of drug release is long, so that the drug cannot take effect quickly after taking it; polyoxyethylene does not have ideal thermal stability, and the dosage The large granulation process is easy to absorb moisture, sticky and difficult to granulate, and the drying temperature requirement is low, and the drying time is long
This causes certain blood drug fluctuations after the drug enters the body

Method used

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  • Nifedipine controlled-release tablet composition and preparation method thereof
  • Nifedipine controlled-release tablet composition and preparation method thereof
  • Nifedipine controlled-release tablet composition and preparation method thereof

Examples

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preparation example Construction

[0036] A preparation method of a nifedipine controlled-release tablet composition, comprising the following steps:

[0037] Step 1, pretreatment: prepare the raw material nifedipine and various auxiliary materials, and micronize the raw material nifedipine under the condition of avoiding light, so that the fineness can pass through a 200-mesh sieve, and the auxiliary materials pass through a 80-100 mesh sieve;

[0038] Step 2, granulation: under dark conditions, dissolve the adhesive in a wetting agent to obtain an adhesive solution, add the raw material nifedipine to the adhesive solution and stir evenly for later use; weigh polyoxyethylene, high The viscous hydrophilic skeleton material, the hydrophobic retarder and the filler are mixed evenly, and then added to the adhesive solution prepared in step 1 to make a soft material; granulation, drying, sizing, adding lubricant and mixing to obtain the granules;

[0039] Step 3, tabletting: under the condition of avoiding light, u...

Embodiment 1

[0042] Granulation: the raw material is micronized and passed through a 200-mesh sieve, the auxiliary material lactose is passed through a 100-mesh sieve, and other auxiliary materials are passed through a 80-mesh sieve; the binder povidone K30 is dissolved in ethanol and the raw material is stirred evenly for later use; the prescription amount of polyoxyethylene is weighed , hypromellose, ethyl cellulose, lactose and or sodium chloride are mixed evenly and added to the prepared binder solution to make a soft material, granulated with a 18-mesh sieve, dried in a hot air circulation oven at 50-60°C, and 18-mesh sieve The whole grain is blended with lubricant magnesium stearate.

[0043] Tablet compression: This step is carried out in the dark, and the granules prepared above are punched with a shallow arc with a diameter of 8.0mm using an ordinary tablet press machine, and the hardness is controlled at 4.0kg / cm 2 up to 12 kg / cm 2 The inspection is qualified and ready for use. ...

Embodiment 2-11

[0046] The nifedipine controlled-release tablet composition of preparation embodiment 2-11 is shown in Table 1 and Table 2,

[0047] Table 1:

[0048]

[0049] Table 2:

[0050]

[0051] Wherein, all numerical values ​​are the dosage of nifedipine per 1000 tablets, and the unit is g, wherein the specification of example 2-example 7 is 30mg / tablet, the specification of example 8-example 9 is 20mg / tablet, and the specification of example 10-example 11 is 60mg / tablet.

[0052] In addition, commercially available Baixintong®, Jiubaoping®, and Xinran® were purchased as control drugs to compare product performance, release, and related substances.

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Abstract

The invention relates to a nifedipine controlled-release tablet composition, comprising the following components in percentage by weight: 4.0-35.0% of nifedipine, 5.0-20.0% of polyoxyethylene, 5.0-30.0% of high-viscosity hydrophilic matrix material, 5.0-20.0% of a hydrophobic retarder, 20.0-60.0% of a filling agent, 0-10.0% of an adhesive solution, and 0.5-1.0% of a lubricant. A preparation method of the composition comprises the following steps: micronizing raw materials under a dark condition until the fineness ensures the powder to pass through a 200-mesh sieve, and screening an auxiliary material through a sieve with 80-100 meshes; adding the medicinal raw materials into the adhesive solution, and stirring uniformly for later use; and weighing a formula amount of polyoxyethylene, hydroxypropyl methylcellulose, the retarder namely ethyl cellulose and the filling agent, mixing uniformly, adding the prepared adhesive solution to prepare a soft material, and performing granulation, drying, straightening, addition of the lubricant, total blending, tabletting and package to obtain the composition. The nifedipine controlled-release tablet composition has the advantages that the preparation process is simple and easy, the production cost is low, and the production cycle is short.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a nifedipine controlled-release tablet composition and a preparation method thereof. Background technique [0002] Nifedipine is the first generation of calcium antagonists. It is an antihypertensive and angina pectoris drug. It is one of the best-selling drugs in the world. Controlled-release preparations can prolong the drug effect time, reduce the peak-valley phenomenon of blood drug concentration, and increase patient compliance, so it is necessary to make nifedipine into controlled-release preparations. Internationally renowned pharmaceutical companies Bayer and Pfizer have both developed nifedipine controlled-release tablets, with trade names of ADALAT® and PROCARDTA respectively. In recent years, Shanghai Modern Pharmaceutical Co., Ltd., Beijing Honglin Pharmaceutical Co., Ltd. and other domestic and foreign pharmaceutical companies are vying to imitate...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4422A61K47/34A61K47/36A61K47/38A61K47/32A61K47/42A61P9/12A61P9/10
CPCA61K9/0002A61K9/2027A61K9/2031A61K9/205A61K9/2054A61K9/2063A61K31/4422
Inventor 刘利清
Owner 浙江为康制药有限公司
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